1sdv | pdb_00001sdv

Crystal structures of HIV protease V82A and L90M mutants reveal changes in indinavir binding site.

spinqualitylabelsall models 1sdv, resolution 1.40Å Show:Asymmetric Unit Biological Assembly Drag the structure with the mouse to rotate   Export Animated Image   Print3D Structural highlights 1sdv is a 2 chain structure with sequence from Human immunodeficiency virus 1. Full crystallographic information is available from OCA. For a guided tour on the structure components use FirstGlance. Ligands: CL, MK1 Related: 1ff0, 1sdt, 1sdu Gene: gag-pol (Human immunodeficiency virus 1) Activity: HIV-1 retropepsin, with EC number 3.4.23.16 Resources: FirstGlance, OCA, RCSB, PDBsum Evolutionary Conservation Check, as determined by ConSurfDB. You may read the explanation of the method and the full data available from ConSurf. Publication Abstract from PubMed The crystal structures of the wild-type HIV-1 protease (PR) and the two resistant variants, PR(V82A) and PR(L90M), have been determined in complex with the antiviral drug, indinavir, to gain insight into the molecular basis of drug resistance. V82A and L90M correspond to an active site mutation and nonactive site mutation, respectively. The inhibition (K(i)) of PR(V82A) and PR(L90M) was 3.3- and 0.16-fold, respectively, relative to the value for PR. They showed only a modest decrease, of 10-15%, in their k(cat)/K(m) values relative to PR. The crystal structures were refined to resolutions of 1.25-1.4 A to reveal critical features associated with inhibitor resistance. PR(V82A) showed local changes in residues 81-82 at the site of the mutation, while PR(L90M) showed local changes near Met90 and an additional interaction with indinavir. These structural differences concur with the kinetic data. Crystal structures of HIV protease V82A and L90M mutants reveal changes in the indinavir-binding site.,Mahalingam B, Wang YF, Boross PI, Tozser J, Louis JM, Harrison RW, Weber IT Eur J Biochem. 2004 Apr;271(8):1516-24. PMID:15066177 From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine. See Also Virus protease

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